Title of article
Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones
Author/Authors
Shuo Zhao، نويسنده , , Yixing Shen، نويسنده , , Arjan van Oeveren، نويسنده , , Keith B. Marschke، نويسنده , , Lin Zhi، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
3431
To page
3435
Abstract
A novel oxachrysenone series (2) of nonsteroidal selective androgen receptor modulators (SARM) was developed based on the 6-aryl-2-quinolinones (1). Synthesis and preliminary SAR results based on in vitro assays are discussed. In the cotransfection assay, lead compound 5d showed AR agonist activity more potent than dihydrotestosterone (DHT), whereas compound 17b was a potent antagonist similar to bicalutamide.
Keywords
androgen receptor , SARM , AR agonist , AR antagonist , Oxachrysen-2-ones
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799574
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